Dihydroergocristine mesylate (DHEC mesylate) is a inhibitor of γ-secretase (GSI), reduces the production of the Alzheimer's disease amyloid-β peptides, binds directly to γ-secretase and Nicastrin with equilibrium dissociation constants (Kd) of 25.7 nM and 9.8 μM, respectively[1].
Dihydroergocristine (DHEC) (2-20 μM; 24 hours) has an IC50 value of 25 μM for inhibiting the activity of γ-secretase in T100 cells without affecting cell viability[1]. Dihydroergocristine (2-20 μM; 24 hours) inhibits cellular Aβ production and causes a dose-dependent accumulation of carboxy-terminal fragments of APP (APP-CTFs) in HEK293 and decreases γ-secretase activity in fibroblast cells[1].
References:
[1]. Lei X, et al. The FDA-approved natural product dihydroergocristine reduces the production of the Alzheimer's disease amyloid-β peptides. Sci Rep. 2015 Nov 16;5:16541.